Design of small molecule ketoamide-based inhibitors of cathepsin K
Design of small molecule ketoamide-based inhibitors of cathepsin K
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DOI：
10.1016/j.bmcl.2003.11.029
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发表时间：
2004-02-09
影响因子：
2.7
通讯作者：
Wright, LL
中科院分区：
文献类型：
--
作者：
Catalano, JG;Deaton, DN;Wright, LL
已经鉴定了一系列新的基于酮酰胺的组织蛋白酶K抑制剂。对p（2）和p（3）元件的修饰对于增强抑制活性是至关重要的。尽管未优化，但在骨吸收的替代测定中，所选抑制剂在减弱1型胶原水解方面是有效的。(C)2003 Elsevier Ltd.保留所有权利。
A novel series of ketoamide-based inhibitors of cathepsin K has been identified. Modifications to p(2) and p(3) elements were crucial to enhancing inhibitory activity. Although not optimized, a selected inhibitor was effective in attenuating type 1 collagen hydrolysis in a surrogate assay of bone resorption. (C) 2003 Elsevier Ltd. All rights reserved.